Ashok Aspatwar, Alessandro Bonardi, Heidi Aisala, Ksenia Zueva, Craig R Primmer, Jaakko Lumme, Seppo Parkkila & Claudiu T. Supuran (2023) Sulphonamide inhibition studies of the β-carbonic anhydrase GsaCAβ present in the salmon platyhelminth parasite Gyrodactylus salaris, Journal of Enzyme Inhibition and Medicinal Chemistry, 38:1, DOI: 10.1080/14756366.2023.2167988
Sulphonamide inhibition studies of the β-carbonic anhydrase GsaCAβ present in the salmon platyhelminth parasite Gyrodactylus salaris
|Author:||Aspatwar, Ashok1; Bonardi, Alessandro2; Aisala, Heidi3;|
1Faculty of Medicine and Health Technology, Tampere University, Tampere, Finland
2Department of Neuroscience, Psychology, Drug Researchand Child’s Health, Section of Pharmaceutical and Nutraceutical Sciences, University of Florence, Sesto Fiorentino, Italy
3Ecology and Genetics,University of Oulu, Oulu, Finland
4Department of Biology, University of Turku, Turku, Finland
5Institute of Biotechnology, University of Helsinki, Helsinki, Finland
6Organismal and Evolutionary Biology Research Programme, University of Helsinki, Helsinki, Finland
7Fimlab Ltd, TampereUniversity Hospital, Tampere, Finland
|Online Access:||PDF Full Text (PDF, 1.5 MB)|
|Persistent link:|| http://urn.fi/urn:nbn:fi-fe2023080994492
|Publish Date:|| 2023-08-09
A β-class carbonic anhydrase (CA, EC 184.108.40.206) present in the genome of the Monogenean platyhelminth Gyrodactylus salaris, a fish parasite, GsaCAβ, has been investigated for its inhibitory effects with a panel of sulphonamides and sulfamates, some of which in clinical use. Several effective GsaCAβ inhibitors were identified, belonging to simple heterocyclic sulphonamides, the deacetylated precursors of acetazolamide and methazolamide (KIsof 81.9–139.7 nM). Many other simple benezene sulphonamides and clinically used agents, such as acetazolamide, methazolamide, ethoxzolamide, dorzolamide, benzolamide, sulthiame and hydrochlorothiazide showed inhibition constants <1 µM. The least effective GsaCAβ inhibitors were 4,6-disubstituted-1,3-benzene disulfonamides, with KIs in the range of 16.9–24.8 µM. Although no potent GsaCAβ-selective inhibitors were detected so far, this preliminary investigation may be helpful for better understanding the inhibition profile of this parasite enzyme and for the potential development of more effective and eventually parasite-selective inhibitors.
Journal of enzyme inhibition and medicinal chemistry
|Type of Publication:||
A1 Journal article – refereed
|Field of Science:||
1181 Ecology, evolutionary biology
This research was financed by the Italian Ministry for Educationand Science (MIUR), grant PRIN: rot. 2017XYBP2R; Ente Cassa diRisparmio di Firenze (ECRF), grant CRF2020.1395 (to CTS);Academy of Finland (to SP); Jane & Aatos Erkko Foundation (toSP); Finnish Cultural Foundation (AA), and Tampere TuberculosisFoundation (AA).
© 2023 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group. This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0/), which permits unrestricted use,distribution, and reproduction in any medium, provided the original work is properly cited.